Icariin
Based on 27 publication(s) in Google Scholar
Icariin is a flavonol glycoside. Icariin inhibits PDE5 and PDE4 activities with IC50s of 432 nM and 73.50 μM, respectively. Icariin also is a PPARα activator.
For research use only. We do not sell to patients.
- Purity: 99.06%
- CAS No.: 489-32-7
- Formula: C33H40O15
- Molecular Weight:676.66
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) Icariin
More- Food Chem. 2025 Dec 30:497:146992. [Abstract]
- Food Chem. 2025 May 31:489:144992. [Abstract]
- Int J Biol Macromol. 2025 Mar 25:142184. [Abstract]
- Phytomedicine. 2025 May:140:156484. [Abstract]
- Phytomedicine. 2024 Sep:132:155901. [Abstract]
- J Ethnopharmacol. 2025 Jan 31:340:119287. [Abstract]
- Int J Mol Sci. 2023 Dec 26;25(1):352. [Abstract]
- Front Pharmacol. 2020 Mar 19;11:256. [Abstract]
- Int Immunopharmacol. 2025 Apr 21:156:114690. [Abstract]
- Int Immunopharmacol. 2024 Jul 30:136:112296. [Abstract]
- RSC Adv. 2025 Sep 29;15(43):35971-35985. [Abstract]
- Exp Neurol. 2025 May 7:115303. [Abstract]
- Mol Divers. 2025 Jan 16. [Abstract]
- Cell Signal. 2025 Dec 18:139:112334. [Abstract]
- Toxicol Appl Pharmacol. 2026 May:510:117761. [Abstract]
- J Neurorestoratology. 2025 Oct.
- J Pharm Pharmacol. 2024 May 3;76(5):499-513. [Abstract]
- J Alzheimers Dis. 2025 Jan 15:13872877241303949. [Abstract]
- J Orthop Surg Res. 2025 Apr 15;20(1):379. [Abstract]
- J Orthop Surg Res. 2025 Mar 18;20(1):290. [Abstract]
- J Orthop Surg Res. 2024 Jul 29;19(1):444. [Abstract]
- J Cell Biochem. 2019 Aug;120(8):13121-13132. [Abstract]
- Biochem Biophys Res Commun. 2024 Nov 12:733:150716. [Abstract]
- Biochem Biophys Res Commun. 2022 Apr 16:600:6-13. [Abstract]
- Arch Dermatol Res. 2024 Aug 23;316(8):557. [Abstract]
- Turk J Gastroenterol. 2021 Apr;32(4):382-392. [Abstract]
- Patent. US20230111925A1.
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Cell Imaging/Staining
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Cell Imaging/Staining
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Cell Imaging/Staining
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WB
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Cell Proliferation/Viability Assay
Biological Activity
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PDE5 432 nM (IC50) |
PDE4 73.5 μM (IC50) |
PPARα |
Autophagy |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| COS-7 | IC50 |
5.9 μM
Compound: 1
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Inhibition of human recombinant PDE5A1 expressed in COS7 cells
Inhibition of human recombinant PDE5A1 expressed in COS7 cells
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[PMID: 18778098] |
| NCI/ADR-RES | IC50 |
>100 μM
Compound: 1, icariin
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Cytotoxicity against human MCF7/ADR cells after 72 hrs by MTT assay
Cytotoxicity against human MCF7/ADR cells after 72 hrs by MTT assay
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[PMID: 19523827] |
| TM3 | CC50 |
>200 μM
Compound: Icariin
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Cytotoxicity against mouse TM3 cells assessed as reduction in cell viability measured after 24 hrs by sulforhodamine B assay
Cytotoxicity against mouse TM3 cells assessed as reduction in cell viability measured after 24 hrs by sulforhodamine B assay
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[PMID: 31091478] |
Icariin is a cGMP-specific PDE5 inhibitor. The inhibitory effects of Icariin on PDE5 and PDE4 activities are investigated by the two-step radioisotope procedure with 3H-cGMP/ 3H-cAMP. The potency of selectivity of Icariin on PDE5 (PDE4/PDE5 of IC50) is 167.67 times[1]. Cell viability is measured in the present study to evaluate whether Icariin protect endothelial HUVECs from injuries induced by oxidized low-density lipoprotein (ox-LDL). The exposure of the cells to ox-LDL for 24 h significantly decreases the cell viability compared with control group (P<0.05). However, Icariin can inhibit cell injury induced by ox-LDL in a concentration-dependent manner, and has significant difference (P<0.05) compared with ox-LDL-simulated group[3].
Icariin protects BMSCs against OGD-induced apoptosis by inhibiting ERs-mediated (ER Stress) autophagy via MAPK signaling pathway[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 489-32-7
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Appearance Solid
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Molecular Weight 676.66
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Formula C33H40O15
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Color Light yellow to yellow
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SMILES
O[C@H]1[C@H](O)[C@@H](CO)O[C@@H](OC2=C(C/C=C(C)/C)C(OC(C3=CC=C(OC)C=C3)=C(O[C@@H]4O[C@@H](C)[C@H](O)[C@@H](O)[C@H]4O)C5=O)=C5C(O)=C2)[C@@H]1O
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Synonyms
Ieariline
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Structure Classification
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Initial Source
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (27)
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Journal Impact Factor
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Most Recent
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Food Chem
Effects of sun drying combined with baking processes on the flavor quality of Chongqing Tuocha raw tea. [Abstract]2025 Dec 30:497:146992. PMID: 41285060 -
Food Chem
Flavonoid-mediated metabolic underpinning quality variation in red bud-sport pear mutants. [Abstract]2025 May 31:489:144992. PMID: 40466530 -
Int J Biol Macromol
Natural angiotensin II type 1 receptor inhibitors: Virtual screening and in vitro evaluation of beta-1,2,3,4,6-penta-O-galloyl-d-glucopyranose, icarrin, and sesamin for osteoarthritis therapy. [Abstract]2025 Mar 25:142184. PMID: 40147655 -
Phytomedicine
Fangchinoline suppresses nasopharyngeal carcinoma progression by inhibiting SQLE to regulate the PI3K/AKT pathway dysregulation. [Abstract]2025 May:140:156484. PMID: 40090046 -
Phytomedicine
Icariin protects against acute graft-versus-host disease while preserving graft-versus-leukemia activity after allogeneic hematopoietic stem cell transplantation. [Abstract]2024 Sep:132:155901. PMID: 39067193 -
J Ethnopharmacol
Icariin maintaining TMEM119-positive microglial population improves hippocampus-associated memory in senescent mice in relation to R-3-hydroxybutyric acid metabolism. [Abstract]2025 Jan 31:340:119287. PMID: 39736348 -
Int J Mol Sci
Icariin Improves Stress Resistance and Extends Lifespan in Caenorhabditis elegans through hsf-1 and daf-2-Driven Hormesis. [Abstract]2023 Dec 26;25(1):352. PMID: 38203522 -
Front Pharmacol
Icariin Ameliorates Diabetic Cardiomyopathy Through Apelin/Sirt3 Signalling to Improve Mitochondrial Dysfunction. [Abstract]2020 Mar 19;11:256. PMID: 32265695
Icariin purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2020 Mar 19;11:256. [Abstract]
As demonstrated by Masson staining, collagen deposition was reduced in the myocardium of Icariin (30 mg/kg)-treated db/db mice.
Icariin purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2020 Mar 19;11:256. [Abstract]
The DHE staining indicated that Icariin (30 mg/kg) treatment alleviated the production of ROS in the myocardial tissue of db/db mice.
Icariin purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2020 Mar 19;11:256. [Abstract]
TUNEL staining revealed that Icariin (30 mg/kg) treatment rescued the apoptotic rate of cardiomyocytes.
Icariin purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2020 Mar 19;11:256. [Abstract]
The mitochondrial dynamics-related protein, Mfn2, mitochondrial biogenesis regulation protein, PGC‐1α, and mitochondrial gene, cytochrome-b (Cyt-b), were upregulated in the Icariin-treated (30 mg/kg) db/db mice.
Icariin purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2020 Mar 19;11:256. [Abstract]
The number of HG-treated cardiomyocytes was significantly higher following incubation with Icariin for 12 h, 24 h, or 48 h at concentrations of 7.5, 15, or 30 µM.
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Int Immunopharmacol
Icariin alleviates cardiomyocyte pyroptosis through AMPK-NLRP3 pathway to ameliorates diabetic cardiomyopathy. [Abstract]2025 Apr 21:156:114690. PMID: 40262250 -
Int Immunopharmacol
Direct targeting of S100A9 with Icariin counteracted acetaminophen‑induced hepatotoxicity. [Abstract]2024 Jul 30:136:112296. PMID: 38810310 -
RSC Adv
Eco-benign spectrofluorimetric analysis of icariin in a nano-formulation using green quantum dots: insights from in vitro anticoagulant and docking studies. [Abstract]2025 Sep 29;15(43):35971-35985. PMID: 41030304 -
Exp Neurol
2025 May 7:115303. PMID: 40345568 -
Mol Divers
Investigating the molecular mechanism of epimedium herb in treating rheumatoid arthritis through network pharmacology, molecular docking, and experimental validation. [Abstract]2025 Jan 16. PMID: 39821498 -
Cell Signal
Icariin attenuates premature ovarian insufficiency via a phytoestrogenic mechanism mediated by the ERβ/SIRT3 pathway. [Abstract]2025 Dec 18:139:112334. PMID: 41421717 -
Toxicol Appl Pharmacol
Icariin regulates osteogenic/adipogenic differentiation of bone marrow mesenchymal stem cells in postmenopausal osteoporosis, potentially via the AMPK-mTOR-autophagy pathway. [Abstract]2026 May:510:117761. PMID: 41702462 -
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J Pharm Pharmacol
Icariside I reduces breast cancer proliferation, apoptosis, invasion, and metastasis probably through inhibiting IL-6/STAT3 signaling pathway. [Abstract]2024 May 3;76(5):499-513. PMID: 37971302 -
J Alzheimers Dis
Icariin improves learning and memory function by enhancing HRD1-mediated ubiquitination of amyloid precursor protein in APP/PS1 mice. [Abstract]2025 Jan 15:13872877241303949. PMID: 39814545 -
J Orthop Surg Res
Investigation on the role of Icariin in tendon injury repair: focusing on tendon stem cell differentiation. [Abstract]2025 Apr 15;20(1):379. PMID: 40234966 -
J Orthop Surg Res
Icariin promotes osteogenic differentiation of bone marrow mesenchymal stem cells (BMSCs) by activating PI3K-AKT-UTX/EZH2 signaling in steroid-induced femoral head osteonecrosis. [Abstract]2025 Mar 18;20(1):290. PMID: 40098175 -
J Orthop Surg Res
The SPI1/SMAD5 cascade in the promoting effect of icariin on osteogenic differentiation of MC3T3-E1 cells: a mechanism study. [Abstract]2024 Jul 29;19(1):444. PMID: 39075522 -
J Cell Biochem
Icariin promotes osteogenic differentiation of bone marrow stromal cells and prevents bone loss in OVX mice via activating autophagy. [Abstract]2019 Aug;120(8):13121-13132. PMID: 30887562 -
Biochem Biophys Res Commun
Icariin alleviates cellular injury induced by cardiac ischemia-reperfusion injury by inhibiting IRE1/JNK-induced ferroptosis. [Abstract]2024 Nov 12:733:150716. PMID: 39321486 -
Biochem Biophys Res Commun
Icariin inhibits RANKL-induced osteoclastogenesis in RAW264.7 cells via inhibition of reactive oxygen species production by reducing the expression of NOX1 and NOX4. [Abstract]2022 Apr 16:600:6-13. PMID: 35182975 -
Arch Dermatol Res
Icariin ameliorates TNF-α/IFN-γ-induced oxidative stress, inflammatory response and apoptosis of human immortalized epidermal cells through the WTAP/SERPINB4 axis. [Abstract]2024 Aug 23;316(8):557. PMID: 39177922 -
Turk J Gastroenterol
Icariin Inhibits Intestinal Inflammation of DSS-Induced Colitis Mice Through Modulating Intestinal Flora Abundance and Modulating p-p65/p65 Molecule. [Abstract]2021 Apr;32(4):382-392. PMID: 34231485 -
Solvent & Solubility
DMSO : 125 mg/mL (184.73 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (3.07 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (3.07 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 10 mg/mL (14.78 mM); Suspended solution; Need ultrasonic
Add each solvent one by one: 0.5% CMC/saline water
Solubility: 10 mg/mL (14.78 mM); Suspended solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
Human umbilical vein endothelial cells (HUVECs) in the logarithmic growth phase are seeded into 96-well plates at a density of 1×104 cells per well, then incubated for 24 hours at 37°C, 5% CO2. After pretreatment with indicated concentration of Icariin (0, 10, 20, 40 μM) for 24 hours, the cells are incubated with or without ox-LDL (100 μg/mL) for next 24 hours. After suction of the liquid in the wells, MTT solution is added to yield a final concentration of 0.5 mg/mL, and incubation is continued for 4 h at 37°C, 5% CO2. MTT solution is removed gently and 150 μL of DMSO is added to each well for 15 min incubation. The absorbance of each sample is measrured on a microplate reader at 490 nm as cell viability[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[2]
Adult 8-week old male C57BL/6 mice are acclimated for 1-week in a temperature- and humidity-controlled facility with a standard 12-h light schedule. Mice have free access to SPF-grade rodent chow and purified drinking water. Mice are treated with Icariin (100, 200, and 400 mg/kg) for 5 days. Clofibrate (CLO, 500 mg/kg, po for 5 days) is used as a positive control, for negative controls, mice are given 2% CMC (10 mL/kg). 24 h after the last dose, livers are collected for analysis.
Rats[4]
Forty adult male SD rats weighing 200-290 g (12-16 weeks old) are randomly assigned to groups (n=10 per group) according to their body weight. The rats receive daily intragastric administration of Icariin at 0 (control), 50, 100, or 200 mg/kg per day for 35 consecutive days. The animals are weighed weekly, and the treatments are adjusted accordingly. At the end of the Icariin treatment period, all rats are sacrificed; blood samples are subsequently collected for further analyses of testosterone levels.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (289 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Xin ZC, et al. Effects of icariin on cGMP-specific PDE5 and cAMP-specific PDE4 activities. Asian J Androl. 2003 Mar;5(1):15-8. [Content Brief]
[2]. Lu YF, et al. Icariin is a PPARα activator inducing lipid metabolic gene expression in mice. Molecules. 2014 Nov 6;19(11):18179-91. [Content Brief]
[3]. Hu Y, et al. Effects and mechanisms of icariin on atherosclerosis. Int J Clin Exp Med. 2015 Mar 15;8(3):3585-9. [Content Brief]
[4]. Chen M, et al. Effects of icariin on reproductive functions in male rats. Molecules. 2014 Jul 3;19(7):9502-14. [Content Brief]
[5]. Liu D, et al. Icariin protects rabbit BMSCs against OGD-induced apoptosis by inhibiting ERs-mediated autophagy via MAPK signaling pathway. Life Sci. 2020 Apr 26:117730. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.4778 mL | 7.3892 mL | 14.7785 mL | 36.9462 mL |
| 5 mM | 0.2956 mL | 1.4778 mL | 2.9557 mL | 7.3892 mL | |
| 10 mM | 0.1478 mL | 0.7389 mL | 1.4778 mL | 3.6946 mL | |
| 15 mM | 0.0985 mL | 0.4926 mL | 0.9852 mL | 2.4631 mL | |
| 20 mM | 0.0739 mL | 0.3695 mL | 0.7389 mL | 1.8473 mL | |
| 25 mM | 0.0591 mL | 0.2956 mL | 0.5911 mL | 1.4778 mL | |
| 30 mM | 0.0493 mL | 0.2463 mL | 0.4926 mL | 1.2315 mL | |
| 40 mM | 0.0369 mL | 0.1847 mL | 0.3695 mL | 0.9237 mL | |
| 50 mM | 0.0296 mL | 0.1478 mL | 0.2956 mL | 0.7389 mL | |
| 60 mM | 0.0246 mL | 0.1232 mL | 0.2463 mL | 0.6158 mL | |
| 80 mM | 0.0185 mL | 0.0924 mL | 0.1847 mL | 0.4618 mL | |
| 100 mM | 0.0148 mL | 0.0739 mL | 0.1478 mL | 0.3695 mL |